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目的借助星点设计-效应面法确定葫芦素口服脂质纳米乳剂的最优处方。方法提出了2个量化乳剂稳定性的常数:灭菌稳定性常数KS和冻融稳定性常数KF。用微射流仪制备葫芦素口服脂质纳米乳剂,采用星点设计-效应面法,以葫芦素口服脂质纳米乳剂的平均粒径(Y1)、灭菌稳定性常数KS(Y2)及冻融稳定性常数KF(Y3)为评价指标,考察了葫芦素口服脂质纳米乳剂处方中聚氧乙烯40氢化蓖麻油的用量(X1)、大豆卵磷脂的用量(X2)及中链脂肪酸甘油三酯的用量(X3)对制剂的影响,以效应面法预测最佳处方。结果优选的最优处方为:m(聚氧乙烯40氢化蓖麻油)∶m(大豆卵磷脂)∶m(中链脂肪酸甘油三酯)=1.15∶0.50∶5.52。采用优化处方制得的葫芦素口服脂质纳米乳剂的平均粒径为(113.6±2.1)nm,灭菌稳定性常数KS为2.92±0.7,冻融稳定性常数KF为5.14±0.2,同预测值的偏差均较低,最大偏差为4.6%。结论星点设计-效应面法所建立的模型能较好地应用于葫芦素口服脂质纳米乳剂处方的优化。
Objective To determine the optimal formulation of cucurbitacin oral lipid nanoemulsion by means of the apical design-response surface method. Methods Two stability constants of quantitative emulsions were proposed: sterility stability constant KS and freezing-thawing stability constant KF. Cucurbitacin oral lipid nanoemulsion was prepared by micro-jet apparatus. The average particle size (Y1), stability constant KS (Y2) and freeze-thaw stability of cucurbitacin oral lipid nanoemulsion were determined by the method of star point design- The stability constant KF (Y3) was used as evaluation index to investigate the effect of cucurbitacin oral lipid nanoemulsion on the dosage of polyoxyethylene 40 hydrogenated castor oil (X1), the amount of soybean lecithin (X2) and medium chain fatty acid triglyceride Dose (X3) on the preparation, the effect of surface area prediction of the best prescription. Results The preferred optimal prescription is: m (polyoxyethylene 40 hydrogenated castor oil): m (soya lecithin): m (medium chain fatty acid triglyceride) = 1.15: 0.50: 5.52. The average particle diameter of cucurbitacin oral lipid nanoemulsion prepared by optimized prescription was (113.6 ± 2.1) nm, the sterilization stability constant KS was 2.92 ± 0.7, the freeze-thaw stability constant KF was 5.14 ± 0.2, The deviation is lower, the maximum deviation of 4.6%. Conclusion The model established by the apical design-response surface method can be applied to the optimization of cucurbitacin oral lipid nanoemulsion formulation.